6BIO

SKU: orb1307114

Description

GSK 3 Inhibitor IX (6-BIO) is a potent, ATP-competitive small molecule that selectively and reversibly inhibits GSK-3α/β (IC50=5 nM) and the CDK1-cyclin B complex. It is widely used in research to study Wnt/β-catenin signaling, neurodevelopment, and cellular proliferation in both in vitro and in vivo models.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 667463-62-9
• MW: 356.18
• Purity: >98%
• Formula: C₁₆H₁₀BrN₃O₂
• SMILES: O\N=C1\C(\Nc2ccccc\12)=C1\C(=O)Nc2cc(Br)ccc12
• Target: Kinase
• Solubility: Soluble in DMSO (up to 15 mg/ml), or in Ethanol (up to 4 mg/ml with warming).

Bioactivity

• Target IC50:
  TYK2:30 nM|CDK5-p35:0.08 μM|GSK-3:5 nM|CDK1-CyclinB:0.32 μM|CDK2-CyclinA:0.30 μM
• In Vivo:
  BIO is a pan-JAK inhibitor targeting TYK2, JAK1, JAK2, and JAK3 with IC50 values of 0.03, 1.5, 8.0, and 0.5 μM, respectively. It also acts as a specific inhibitor of glycogen synthase kinase-3 (GSK-3), with an IC50 of 5 nM for GSK-3α/β, demonstrating over 16-fold higher selectivity than for CDK5. BIO interacts with the ATP-binding pockets of these kinases, reducing phosphorylation at GSK-3 specific sites on β-catenin in cell models and promoting the proliferation of mammalian cardiomyocytes. Moreover, BIO selectively inhibits STAT3 phosphorylation, inducing apoptosis in human melanoma cells. In human and mouse embryonic stem cells, BIO preserves the undifferentiated phenotype and maintains the expression of pluripotency-specific transcription factors Oct-3/4, Rex-1, and Nanog.
• In Vitro:
  BIO inhibits the growth of melanoma in murine xenograft models.
• Cell Research:
  COS1, Hepa (wild-type, CEM/LM AhR deficient and ELB1 ARNT deficient), or SH-SY5Y cells are grown in 6 cm culture dishes in Dulbecco's Modified Medium (DMEM) containing 10% fetal bovine serum. For treatment, IO (5 μM), BIO (5 or 10 μM), MeBIO (5 or 50 μM), LiCl (20 or 40 mM), or mock solution (DMSO, 0.5% final concentration) is added to medium when cell density reaches ～70% confluence. After 12 (SH-SY5Y) or 24 hours, the cells, while still in plate, are lysed with lysis buffer (1% SDS, 1 mM sodium orthovanadate, 10 mM Tris [pH 7.4]). The lysate is passed several times through a 26 g needle, centrifuged at 10,000 × g for 5 min, and adjusted to equal protein concentration. About 8 μg of each sample is loaded for immunoblotting. Enhanced chemiluminescence is used for detection. The following primary antibodies are used: mouse anti-β-catenin CT (Upstate Biotechnolgies, Clone 7D8, recognizes total β-catenin), mouse anti-phospho-β-catenin (Upstate Biotechnologies, Clone 8E7, recognizes dephosphorylated β-catenin), mouse anti-GSK-3 β, mouse anti-GSK-3 phosphoTyr216, rabbit anti-AhR (Aryl hydrocarbon receptor), and rabbit anti-actin.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK5/p35, CDK1/CyclinB, CDK2/CyclinA, CDK, BIO, Apoptosis, 6-Bromoindirubin-3'-oxime, 6-bromoindirubin-3-oxime, 6-BIO, GSK-3, GSK3, GSK 3 Inhibitor IX, GSK 3 IX, MLS 2052, MLS2052, MLS-2052, Tyrosine Kinases, TyrosineKinases, Tyk2

Compound Identifiers

PubChem CID

448949